Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold
文献类型：期刊论文
| 作者 | Zhu, Junjie1; Ning, Mengmeng1 ; Guo, Cen2; Zhang, Lina1; Pan, Guoyu2; Leng, Ying1; Shen, Jianhua1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2013-11 |
| 卷号 | 69页码:55-68 |
| 关键词 | TGR5 GPCR Diabetes 4-Phenyl pyridine |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2013.07.050 |
| 文献子类 | Article |
| 英文摘要 | TGR5, a GPCR, is involved in energy and glucose homeostasis, and as such, is a target for the treatment of diabetes, obesity and other metabolic syndromes. A new class of TGR5 agonists based on a 4-phenyl pyridine scaffold was designed, synthesized and evaluated in vitro and in vivo. Extensive structure activity relationship studies are reported herein. The most potent compounds 15a, 18b and 18c showed comparable activity with the lead compound 2. 15a had the best potency in vitro but displayed an pharmacokinetic profile and was found to be ineffective during an oral glucose tolerance test in imprinting control region mice at a dose of 50 mg/kg. (C) 2013 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | BILE-ACIDS ; RECEPTOR ; DERIVATIVES ; ALCOHOLS |
| 资助项目 | National Science and Technology Major Project-Key New Drug Creation and Manufacturing Program, China[2012ZX09103101-049] ; National Nature Science Foundation of China[81202571] ; National Science and Technology Major Project[2012ZX09301001-006] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000330603900006 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277384]  |
| 专题 | 药理学第一研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 药物发现与设计中心 |
| 通讯作者 | Leng, Ying |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Ctr Drug Safety Evaluat & Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhu, Junjie,Ning, Mengmeng,Guo, Cen,et al. Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2013,69:55-68. |
| APA | Zhu, Junjie.,Ning, Mengmeng.,Guo, Cen.,Zhang, Lina.,Pan, Guoyu.,...&Shen, Jianhua.(2013).Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,69,55-68. |
| MLA | Zhu, Junjie,et al."Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 69(2013):55-68. |
入库方式： OAI收割
来源：上海药物研究所
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